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Conversion of a non-selective adenosine receptor antagonist into A3-selective high affinity fluorescent probes using peptide-based linkers.

Vernall AJ, Stoddart LA, Briddon SJ, Ng HW, Laughton CA, Doughty SW, Hill SJ, Kellam B.

Org Biomol Chem. 2013 Sep 14;11(34):5673-82. doi: 10.1039/c3ob41221k.


Highly potent and selective fluorescent antagonists of the human adenosine A₃ receptor based on the 1,2,4-triazolo[4,3-a]quinoxalin-1-one scaffold.

Vernall AJ, Stoddart LA, Briddon SJ, Hill SJ, Kellam B.

J Med Chem. 2012 Feb 23;55(4):1771-82. doi: 10.1021/jm201722y. Epub 2012 Feb 13.


Influence of fluorophore and linker composition on the pharmacology of fluorescent adenosine A1 receptor ligands.

Baker JG, Middleton R, Adams L, May LT, Briddon SJ, Kellam B, Hill SJ.

Br J Pharmacol. 2010 Feb;159(4):772-86. doi: 10.1111/j.1476-5381.2009.00488.x. Epub 2010 Jan 26.


Discovery of simplified N²-substituted pyrazolo[3,4-d]pyrimidine derivatives as novel adenosine receptor antagonists: efficient synthetic approaches, biological evaluations and molecular docking studies.

Venkatesan G, Paira P, Cheong SL, Vamsikrishna K, Federico S, Klotz KN, Spalluto G, Pastorin G.

Bioorg Med Chem. 2014 Mar 1;22(5):1751-65. doi: 10.1016/j.bmc.2014.01.018. Epub 2014 Jan 31.


Fluorescent ligands for adenosine receptors.

Kozma E, Jayasekara PS, Squarcialupi L, Paoletta S, Moro S, Federico S, Spalluto G, Jacobson KA.

Bioorg Med Chem Lett. 2013 Jan 1;23(1):26-36. doi: 10.1016/j.bmcl.2012.10.112. Epub 2012 Nov 5. Review.


Functionalized congener approach to the design of ligands for G protein-coupled receptors (GPCRs).

Jacobson KA.

Bioconjug Chem. 2009 Oct 21;20(10):1816-35. doi: 10.1021/bc9000596. Epub 2009 Apr 30. Review.


Agonist-occupied A3 adenosine receptors exist within heterogeneous complexes in membrane microdomains of individual living cells.

Cordeaux Y, Briddon SJ, Alexander SP, Kellam B, Hill SJ.

FASEB J. 2008 Mar;22(3):850-60. Epub 2007 Oct 24.


Design and use of fluorescent ligands to study ligand-receptor interactions in single living cells.

Briddon SJ, Kellam B, Hill SJ.

Methods Mol Biol. 2011;746:211-36. doi: 10.1007/978-1-61779-126-0_11.


Exploring a 2-naphthoic acid template for the structure-based design of P2Y14 receptor antagonist molecular probes.

Kiselev E, Barrett MO, Katritch V, Paoletta S, Weitzer CD, Brown KA, Hammes E, Yin AL, Zhao Q, Stevens RC, Harden TK, Jacobson KA.

ACS Chem Biol. 2014 Dec 19;9(12):2833-42. doi: 10.1021/cb500614p. Epub 2014 Oct 20.


Limits of ligand selectivity from docking to models: in silico screening for A(1) adenosine receptor antagonists.

Kolb P, Phan K, Gao ZG, Marko AC, Sali A, Jacobson KA.

PLoS One. 2012;7(11):e49910. doi: 10.1371/journal.pone.0049910. Epub 2012 Nov 21.


Fragment screening at adenosine-A(3) receptors in living cells using a fluorescence-based binding assay.

Stoddart LA, Vernall AJ, Denman JL, Briddon SJ, Kellam B, Hill SJ.

Chem Biol. 2012 Sep 21;19(9):1105-15. doi: 10.1016/j.chembiol.2012.07.014.


Synthesis and characterization of selective fluorescent ligands for the neurokinin NK2 receptor.

Bradshaw CG, Ceszkowski K, Turcatti G, Beresford IJ, Chollet A.

J Med Chem. 1994 Jun 24;37(13):1991-5.


Synthesis, CoMFA analysis, and receptor docking of 3,5-diacyl-2, 4-dialkylpyridine derivatives as selective A3 adenosine receptor antagonists.

Li AH, Moro S, Forsyth N, Melman N, Ji XD, Jacobson KA.

J Med Chem. 1999 Feb 25;42(4):706-21.


7-Nitrobenzofurazan (NBD) derivatives of 5'-N-ethylcarboxamidoadenosine (NECA) as new fluorescent probes for human A(3) adenosine receptors.

Macchia M, Salvetti F, Bertini S, Di Bussolo V, Gattuso L, Gesi M, Hamdan M, Klotz KN, Laragione T, Lucacchini A, Minutolo F, Nencetti S, Papi C, Tuscano D, Martini C.

Bioorg Med Chem Lett. 2001 Dec 3;11(23):3023-6.


Environment and mobility of a series of fluorescent reporters at the amino terminus of structurally related peptide agonists and antagonists bound to the cholecystokinin receptor.

Harikumar KG, Pinon DI, Wessels WS, Prendergast FG, Miller LJ.

J Biol Chem. 2002 May 24;277(21):18552-60. Epub 2002 Mar 13.


Synthesis and characterization of fluorescent antagonists and agonists for human oxytocin and vasopressin V(1)(a) receptors.

Terrillon S, Cheng LL, Stoev S, Mouillac B, Barberis C, Manning M, Durroux T.

J Med Chem. 2002 Jun 6;45(12):2579-88.


Characterization by flow cytometry of fluorescent, selective agonist probes of the A(3) adenosine receptor.

Kozma E, Gizewski ET, Tosh DK, Squarcialupi L, Auchampach JA, Jacobson KA.

Biochem Pharmacol. 2013 Apr 15;85(8):1171-81. doi: 10.1016/j.bcp.2013.01.021. Epub 2013 Jan 31.


New fluorescent adenosine A1-receptor agonists that allow quantification of ligand-receptor interactions in microdomains of single living cells.

Middleton RJ, Briddon SJ, Cordeaux Y, Yates AS, Dale CL, George MW, Baker JG, Hill SJ, Kellam B.

J Med Chem. 2007 Feb 22;50(4):782-93. Epub 2007 Jan 24.

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